DE60018215T2 - Verbindungen und verfahren zur modulation von estrogen rezeptoren - Google Patents

Verbindungen und verfahren zur modulation von estrogen rezeptoren Download PDF

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Publication number
DE60018215T2
DE60018215T2 DE60018215T DE60018215T DE60018215T2 DE 60018215 T2 DE60018215 T2 DE 60018215T2 DE 60018215 T DE60018215 T DE 60018215T DE 60018215 T DE60018215 T DE 60018215T DE 60018215 T2 DE60018215 T2 DE 60018215T2
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DE
Germany
Prior art keywords
compound according
compound
compounds
estrogen
heterocycle
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
DE60018215T
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German (de)
English (en)
Other versions
DE60018215D1 (de
Inventor
S. Shripad BHAGWAT
A. Jeffrey MCKIE
Sak Khammungkhune
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Signal Pharmaceuticals LLC
Original Assignee
Signal Pharmaceuticals LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/492,939 external-priority patent/US6291456B1/en
Priority claimed from US09/611,156 external-priority patent/US6331562B1/en
Application filed by Signal Pharmaceuticals LLC filed Critical Signal Pharmaceuticals LLC
Publication of DE60018215D1 publication Critical patent/DE60018215D1/de
Application granted granted Critical
Publication of DE60018215T2 publication Critical patent/DE60018215T2/de
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/06Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
    • C07D311/08Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
    • C07D311/16Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted in position 7

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Reproductive Health (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
DE60018215T 1999-12-30 2000-12-29 Verbindungen und verfahren zur modulation von estrogen rezeptoren Expired - Fee Related DE60018215T2 (de)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US47577699A 1999-12-30 1999-12-30
US475776 1999-12-30
US09/492,939 US6291456B1 (en) 1998-12-30 2000-01-27 Compounds and methods for modulation of estrogen receptors
US492939 2000-01-27
US611156 2000-07-06
US09/611,156 US6331562B1 (en) 1998-12-30 2000-07-06 Compounds and methods for modulation of estrogen receptors
PCT/US2000/035671 WO2001049673A2 (en) 1999-12-30 2000-12-29 Compounds and methods for modulation of estrogen receptors

Publications (2)

Publication Number Publication Date
DE60018215D1 DE60018215D1 (de) 2005-03-24
DE60018215T2 true DE60018215T2 (de) 2006-02-09

Family

ID=27413348

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60018215T Expired - Fee Related DE60018215T2 (de) 1999-12-30 2000-12-29 Verbindungen und verfahren zur modulation von estrogen rezeptoren

Country Status (13)

Country Link
EP (1) EP1246814B1 (enExample)
JP (1) JP2003519219A (enExample)
KR (1) KR20020075388A (enExample)
CN (1) CN1281598C (enExample)
AT (1) ATE289300T1 (enExample)
AU (1) AU781282B2 (enExample)
CA (1) CA2396059A1 (enExample)
DE (1) DE60018215T2 (enExample)
DK (1) DK1246814T3 (enExample)
ES (1) ES2238034T3 (enExample)
IL (1) IL150463A0 (enExample)
PT (1) PT1246814E (enExample)
WO (1) WO2001049673A2 (enExample)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CO5271709A1 (es) * 2000-01-12 2003-04-30 Pfizer Prod Inc Composiciones y procedimientos para el y tratamiento de afecciones que responden a estrogenos
EP1177787A3 (en) * 2000-07-28 2003-09-10 Pfizer Products Inc. Use of an estrogen agonist/antagonist for treating cataracts
EP1281710A1 (en) * 2001-08-03 2003-02-05 CHIESI FARMACEUTICI S.p.A. 2H-1-benzopyran derivatives, processes for their preparation and pharmaceutical compositions thereof
US7148252B2 (en) * 2001-10-03 2006-12-12 Signal Pharmaceuticals, Llc Use of benzopyranones for treating or preventing a primary brain cancer or a brain metastasis
US7217734B2 (en) 2001-11-19 2007-05-15 Eli Lilly And Company Substituted benzopyrans as selective estrogen receptor-beta agonists
US7524866B2 (en) 2001-11-29 2009-04-28 Gtx, Inc. Prevention and treatment of androgen—deprivation induced osteoporosis
WO2003047504A2 (en) * 2001-11-29 2003-06-12 Gtx Inc. Prevention and treatment of androgen-deprivation induced osteoporosis
AU2005202072B2 (en) * 2001-11-29 2008-10-23 Gtx, Inc. Prevention and treatment of androgen-deprivation induced conditions
AU2003239155B2 (en) * 2002-04-19 2008-12-04 Novartis Ag Benzopyranone compounds, compositions thereof, and methods of treatment therewith
US7091235B2 (en) 2002-10-15 2006-08-15 Signal Pharmaceuticals, Llc Benzopyranone compounds, compositions thereof, and methods for treating or preventing cancer
US7674783B2 (en) * 2002-11-22 2010-03-09 Dimera Inc. Estrogen beta receptor agonists to prevent or reduce the severity of cardiovascular disease
MXPA05011243A (es) 2003-04-21 2005-12-15 Lilly Co Eli Benzopiranos substituidos como agonistas selectivos del receptor beta de estrogeno.
ES2338119T3 (es) 2003-04-21 2010-05-04 Eli Lilly And Company Benzopiranos sustituidos como agonistas selectivos del receptor-beta de estrogeno.
US7098340B2 (en) * 2003-05-14 2006-08-29 Warner Lambert Company Llc Benzyl sulfonamide derivatives
WO2005028472A1 (en) * 2003-09-15 2005-03-31 Signal Pharmaceuticals, Llc Benzopyranone compounds, compositions thereof, and methods of treatment therewith
CA2595472A1 (en) * 2005-01-21 2006-07-27 Janssen Pharmaceutica N.V. Novel coumarin derivatives as ion channel openers
WO2008002490A2 (en) * 2006-06-23 2008-01-03 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
PL2568806T3 (pl) 2010-05-12 2017-03-31 Radius Health, Inc. Schematy lecznicze
EP2621901B1 (en) 2010-09-28 2015-07-29 Radius Health, Inc Selective androgen receptor modulators
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
SI3122426T1 (sl) 2014-03-28 2023-04-28 Duke University Zdravljenje raka dojk z uporabo selektivnih modulatorjev estrogenskih receptorjev
CN105801544A (zh) * 2016-04-18 2016-07-27 中国药科大学 3-芳基-4-芳香胺-香豆素衍生物及其制备方法和医药用途
CN105801543B (zh) * 2016-04-18 2019-08-02 中国药科大学 4-芳香胺-香豆素衍生物及其制备方法和医药用途
PT3474841T (pt) 2016-06-22 2022-06-20 Radius Health Inc Métodos de tratamento do cancro de mama ar+
CN106492204A (zh) * 2016-12-27 2017-03-15 郑州郑先医药科技有限公司 一种治疗白内障的药物组合物
CN106727637A (zh) * 2016-12-27 2017-05-31 郑州郑先医药科技有限公司 一种治疗白内障的西药组合物及其用途
EP3565542B1 (en) 2017-01-05 2024-04-10 Radius Pharmaceuticals, Inc. Polymorphic forms of rad1901-2hcl

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5883118A (en) * 1996-01-11 1999-03-16 Nova Nordisk A/S Prostatic carcinoma
US5726202A (en) * 1996-01-11 1998-03-10 Novo Nordisk A/S Benign prostatic hypertrophy
IL124882A0 (en) * 1996-01-11 1999-01-26 Novo Nordisk As Use of 3, 4-diphenyl chromans for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of menopausal symptoms
ATE248157T1 (de) * 1998-12-30 2003-09-15 Signal Pharm Inc Verbindungen und verfahren zur modulation von estrogen rezeptoren

Also Published As

Publication number Publication date
DE60018215D1 (de) 2005-03-24
CN1437591A (zh) 2003-08-20
CN1281598C (zh) 2006-10-25
DK1246814T3 (da) 2005-05-30
IL150463A0 (en) 2002-12-01
WO2001049673A2 (en) 2001-07-12
EP1246814B1 (en) 2005-02-16
EP1246814A2 (en) 2002-10-09
AU3077101A (en) 2001-07-16
AU781282B2 (en) 2005-05-12
WO2001049673A3 (en) 2001-12-06
HK1058521A1 (en) 2004-05-21
ATE289300T1 (de) 2005-03-15
ES2238034T3 (es) 2005-08-16
KR20020075388A (ko) 2002-10-04
CA2396059A1 (en) 2001-07-12
JP2003519219A (ja) 2003-06-17
PT1246814E (pt) 2005-07-29

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Owner name: SIGNAL PHARMACEUTICALS LLC, SAN DIEGO, CALIF., US

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8339 Ceased/non-payment of the annual fee